Platinum drugs are widely used in cancer therapy, because they induce apoptosis by damaging nuclear DNA in cancer cells. Among the platinum drugs, cisplatin, carboplatin, and oxaliplatin have FDA approval and are clinically used in the United States and elsewhere. The use of platinum(II) drugs in the treatment of malignancies has been somewhat limited because of the side effects and resistance acquired by cancer cells. An alternative to platinum(II) drug candidates is the use of substitutionally more inert platinum(IV) compounds as prodrugs derived from clinically effective platinum(II) compounds. Substitutionally inert platinum(IV) complexes are less likely to be deactivated prior to reaching their destination target in the cancer cell. The activity of platinum(IV) complexes generally involves reduction with concomitant loss of the axial ligands, affording an active platinum(II) complex that readily binds to DNA. The axial ligands which are released from the platinum(IV) complex may comprise a therapeutically active agent with the same or different mechanism of action as the resulting platinum(II) drug. Single agents with dual targeting capabilities provide a powerful approach to treating cancer. Therefore, it would be beneficial to have methods, compounds, and compositions for treating cancer using a single platinum(IV) agent with dual targeting capabilities.